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PF-03654746

Chemical Structure : PF-03654746

CAS No.: 935840-31-6

PF-03654746 (PF-3654746, PF03654746)

Catalog No.: PC-63034Not For Human Use, Lab Use Only.

PF-03654746 (PF-3654746) is a potent, selective, orally bioactive antagonist of H3 receptor with Ki of 2.3 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    PF-03654746 (PF-3654746) is a potent, selective, orally bioactive antagonist of H3 receptor with Ki of 2.3 nM.
    PF-03654746 dislaplays >1000-fold selectivity versus H1, H2, H4 and other GPCRs (IC50>10 uM).
    PF-03654746 possesses optimal pharmacological and pharmacokinetic profiles, shows potential in allergen-induced nasal symptoms.

    Physicochemical Properties

    M.Wt 322.4
    Formula C18H24F2N2O
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    Trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide

    References

    1. Wager TT, et al. J Med Chem. 2011 Nov 10;54(21):7602-20.

    2. Stokes JR, et al. J Allergy Clin Immunol. 2012 Feb;129(2):409-12, 412.e1-2.

    3. Gallezot JD, et al. J Cereb Blood Flow Metab. 2017 Mar;37(3):1095-1107.

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